Target Information
| Target General Information | Top | |||||
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| Target ID |
T51487
(Former ID: TTDS00403)
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| Target Name |
GABA(A) receptor alpha-1 (GABRA1)
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| Synonyms |
Gamma-aminobutyric acid receptor subunit alpha-1; GABA(A) receptor subunit alpha-1
Click to Show/Hide
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| Gene Name |
GABRA1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 13 Target-related Diseases | + | ||||
| 1 | Acute respiratory distress syndrome [ICD-11: CB00] | |||||
| 2 | Anxiety disorder [ICD-11: 6B00-6B0Z] | |||||
| 3 | Chronic insomnia [ICD-11: 7A00] | |||||
| 4 | Chronic pain [ICD-11: MG30] | |||||
| 5 | Corneal disease [ICD-11: 9A76-9A78] | |||||
| 6 | Cystitis [ICD-11: GC00] | |||||
| 7 | Depression [ICD-11: 6A70-6A7Z] | |||||
| 8 | Epilepsy/seizure [ICD-11: 8A61-8A6Z] | |||||
| 9 | Headache [ICD-11: 8A80-8A84] | |||||
| 10 | Insomnia [ICD-11: 7A00-7A0Z] | |||||
| 11 | Malaria [ICD-11: 1F40-1F45] | |||||
| 12 | Mental/behavioural/neurodevelopmental disorder [ICD-11: 6E20-6E8Z] | |||||
| 13 | Tonus and reflex abnormality [ICD-11: MB47] | |||||
| Function |
Ligand-gated chloride channel which is a component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the brain. Plays an important role in the formation of functional inhibitory GABAergic synapses in addition to mediating synaptic inhibition as a GABA-gated ion channel. The gamma2 subunit is necessary but not sufficient for a rapid formation of active synaptic contacts and the synaptogenic effect of this subunit is influenced by the type of alpha and beta subunits present in the receptor pentamer (By similarity). The alpha1/beta2/gamma2 receptor and the alpha1/beta3/gamma2 receptor exhibit synaptogenic activity. GABRA1-mediated plasticity in the orbitofrontal cortex regulates context-dependent action selection (By similarity). Functions also as histamine receptor and mediates cellular responses to histamine (By similarity).
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| BioChemical Class |
Ligand-gated ion channel
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| UniProt ID | ||||||
| Sequence |
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T93QP3 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 22 Approved Drugs | + | ||||
| 1 | Allopregnanolone | Drug Info | Approved | Postpartum depression | [6], [7] | |
| 2 | Amobarbital | Drug Info | Approved | Insomnia | [3], [8] | |
| 3 | Barbital | Drug Info | Approved | Insomnia | [1] | |
| 4 | Butabarbital | Drug Info | Approved | Insomnia | [9], [10] | |
| 5 | Butalbital | Drug Info | Approved | Anxiety disorder | [3], [11], [12] | |
| 6 | Butethal | Drug Info | Approved | Insomnia | [13] | |
| 7 | Clobazam - Lundbeck | Drug Info | Approved | Anxiety disorder | [14], [15] | |
| 8 | Ethanol | Drug Info | Approved | Cystitis | [3], [16], [17] | |
| 9 | Ethchlorvynol | Drug Info | Approved | Insomnia | [18], [19] | |
| 10 | Hexobarbital | Drug Info | Approved | Anaesthesia | [20] | |
| 11 | Indiplon | Drug Info | Approved | Insomnia | [21], [22] | |
| 12 | Methohexital | Drug Info | Approved | Anaesthesia | [23], [24] | |
| 13 | Methoxyflurane | Drug Info | Approved | Anaesthesia | [25], [26] | |
| 14 | Methylphenobarbital | Drug Info | Approved | Anxiety disorder | [27] | |
| 15 | Methyprylon | Drug Info | Approved | Insomnia | [28], [29] | |
| 16 | Nitrazepam | Drug Info | Approved | Epilepsy | [30], [3] | |
| 17 | Pentobarbital | Drug Info | Approved | Insomnia | [3], [31], [32] | |
| 18 | Picrotoxin | Drug Info | Approved | Respiratory distress syndrome | [33], [34] | |
| 19 | Secobarbital | Drug Info | Approved | Intractable insomnia | [3] | |
| 20 | THIOCOLCHICOSIDE | Drug Info | Approved | Muscle spasm | [3] | |
| 21 | Zaleplon | Drug Info | Approved | Insomnia | [35], [36] | |
| 22 | Zolpidem | Drug Info | Approved | Insomnia | [37], [3] | |
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | ZK-93423 | Drug Info | Phase 3 | Epileptic seizures | [38], [39] | |
| 2 | EVT-201 | Drug Info | Phase 2 | Insomnia | [40] | |
| 3 | GSK683699 | Drug Info | Phase 2 | Inflammatory bowel disease | [41] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | ELTANOLONE | Drug Info | Discontinued in Phase 3 | Premenstrual syndrome | [42] | |
| 2 | U-78875 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [43] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Inhibitor | [+] 155 Inhibitor drugs | + | ||||
| 1 | Allopregnanolone | Drug Info | [44] | |||
| 2 | THIOCOLCHICOSIDE | Drug Info | [48] | |||
| 3 | ZK-93423 | Drug Info | [51] | |||
| 4 | GSK683699 | Drug Info | [48] | |||
| 5 | ELTANOLONE | Drug Info | [44] | |||
| 6 | U-78875 | Drug Info | [52] | |||
| 7 | Divaplon | Drug Info | [53] | |||
| 8 | (2-Amino-4,5-dihydro-thiazol-4-yl)-acetic acid | Drug Info | [54] | |||
| 9 | (2E,4S)-4-ammoniopent-2-enoate | Drug Info | [55] | |||
| 10 | (4R)-4-ammoniopentanoate | Drug Info | [55] | |||
| 11 | (4S)-4-ammoniopentanoate | Drug Info | [55] | |||
| 12 | (6-Benzylamino-9H-beta-carbolin-3-yl)-methanol | Drug Info | [56] | |||
| 13 | (9-Benzyl-9H-purin-6-yl)-cyclopropyl-amine | Drug Info | [57] | |||
| 14 | (9H-beta-Carbolin-3-yl)-carbamic acid ethyl ester | Drug Info | [58] | |||
| 15 | (9H-beta-Carbolin-3-yl)-ethyl-amine | Drug Info | [58] | |||
| 16 | (9H-beta-Carbolin-3-yl)-methanol | Drug Info | [56] | |||
| 17 | (beta-CCE)9H-beta-Carboline-3-carboxylic acid | Drug Info | [59] | |||
| 18 | 1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one | Drug Info | [60] | |||
| 19 | 1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one | Drug Info | [61] | |||
| 20 | 1-(4-chlorophenyl)-4-phenyl-1H-imidazole | Drug Info | [62] | |||
| 21 | 1-(9H-beta-Carbolin-3-yl)-ethanone | Drug Info | [56] | |||
| 22 | 1-Methyl-5-oxa-spiro[2.4]heptan-4-one | Drug Info | [60] | |||
| 23 | 2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide | Drug Info | [59] | |||
| 24 | 2-(3-Bromo-phenyl)-6-nitro-chromen-4-one | Drug Info | [63] | |||
| 25 | 2-(3-Bromo-phenyl)-chromen-4-one | Drug Info | [63] | |||
| 26 | 2-(3-Chloro-phenyl)-chromen-4-one | Drug Info | [63] | |||
| 27 | 2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one | Drug Info | [62] | |||
| 28 | 2-(9-Benzyl-9H-purin-6-ylamino)-ethanol | Drug Info | [57] | |||
| 29 | 2-Furan-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one | Drug Info | [64] | |||
| 30 | 2-Isoxazol-3-yl-3H-imidazo[4,5-c]quinoline | Drug Info | [65] | |||
| 31 | 2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline | Drug Info | [65] | |||
| 32 | 2-p-Tolyl-6H-pyrazolo[1,5-c]quinazolin-5-one | Drug Info | [64] | |||
| 33 | 2-Phenyl-5,6-dihydro-pyrazolo[1,5-c]quinazoline | Drug Info | [64] | |||
| 34 | 2-Phenyl-6H-pyrazolo[1,5-c]quinazolin-5-one | Drug Info | [64] | |||
| 35 | 2-Pyridin-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one | Drug Info | [64] | |||
| 36 | 2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline | Drug Info | [65] | |||
| 37 | 3,3-Diethyl-dihydro-furan-2-one | Drug Info | [60] | |||
| 38 | 3,3-Diisopropyl-dihydro-furan-2-one | Drug Info | [60] | |||
| 39 | 3-(2,2-Dimethyl-propoxy)-9H-beta-carboline | Drug Info | [66] | |||
| 40 | 3-(3-Methyl-butoxy)-9H-beta-carboline | Drug Info | [66], [67] | |||
| 41 | 3-(benzyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [67] | |||
| 42 | 3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [67] | |||
| 43 | 3-amino-3-demethoxythiocolchicine | Drug Info | [48] | |||
| 44 | 3-Butoxy-9H-beta-carboline | Drug Info | [66], [67] | |||
| 45 | 3-butoxycarbonyl-4-quinolone | Drug Info | [68] | |||
| 46 | 3-butoxycarbonyl-6-ethyl-4-quinolone | Drug Info | [68] | |||
| 47 | 3-carboxy-6-ethyl-4-quinolone | Drug Info | [68] | |||
| 48 | 3-Chloro-9H-beta-carboline | Drug Info | [69] | |||
| 49 | 3-cyclopentoxycarbonyl-6-ethyl-4-quinolone | Drug Info | [68] | |||
| 50 | 3-demethoxy-3-D-lyxopyranosylaminothiocolchicine | Drug Info | [48] | |||
| 51 | 3-demethoxy-3-D-mannopyranosylaminothiocolchicine | Drug Info | [48] | |||
| 52 | 3-demethoxy-3-D-xylopyranosylaminothiocolchicine | Drug Info | [48] | |||
| 53 | 3-demethoxy-3-L-fucopyranosylaminothiocolchicine | Drug Info | [48] | |||
| 54 | 3-demethoxy-3D-glucopyranosylaminothiocolchicine | Drug Info | [48] | |||
| 55 | 3-Ethoxy-9H-beta-carboline | Drug Info | [69], [67] | |||
| 56 | 3-ethoxycarbonyl-4-quinolone | Drug Info | [68] | |||
| 57 | 3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone | Drug Info | [68] | |||
| 58 | 3-ethoxycarbonyl-6-propyl-4-quinolone | Drug Info | [68] | |||
| 59 | 3-Ethyl-3-isopropyl-dihydro-furan-2-one | Drug Info | [60] | |||
| 60 | 3-Ethyl-3-methyl-dihydro-furan-2-one | Drug Info | [60] | |||
| 61 | 3-Isobutoxy-9H-beta-carboline | Drug Info | [66], [67] | |||
| 62 | 3-Isopropoxy-9H-beta-carboline | Drug Info | [66] | |||
| 63 | 3-Isopropyl-3-methyl-dihydro-furan-2-one | Drug Info | [60] | |||
| 64 | 3-Isothiocyanato-9H-beta-carboline | Drug Info | [70] | |||
| 65 | 3-Methoxy-9H-beta-carboline | Drug Info | [69] | |||
| 66 | 3-Methoxycarbonyl-2-methyl-9H-beta-carbolin-2-ium | Drug Info | [71] | |||
| 67 | 3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one | Drug Info | [61] | |||
| 68 | 3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one | Drug Info | [61] | |||
| 69 | 3-Methyl-9H-beta-carboline | Drug Info | [72] | |||
| 70 | 3-Nitro-9H-beta-carboline | Drug Info | [69] | |||
| 71 | 3-Propoxy-9H-beta-carboline | Drug Info | [69], [67] | |||
| 72 | 3-sec-Butoxy-9H-beta-carboline | Drug Info | [66] | |||
| 73 | 3-tert-Butyl-3-ethyl-dihydro-furan-2-one | Drug Info | [60] | |||
| 74 | 4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol | Drug Info | [73] | |||
| 75 | 4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole | Drug Info | [62] | |||
| 76 | 4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol | Drug Info | [74] | |||
| 77 | 4-benzyl-5-(4-piperidyl)isothiazol-3-ol | Drug Info | [75] | |||
| 78 | 4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol | Drug Info | [76] | |||
| 79 | 4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline | Drug Info | [77] | |||
| 80 | 4-Methyl-5-(4-piperidyl)isothiazol-3-ol | Drug Info | [75] | |||
| 81 | 4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol | Drug Info | [76] | |||
| 82 | 4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol | Drug Info | [76] | |||
| 83 | 5-(4-piperidyl)-4-propylisothiazol-3-ol | Drug Info | [75] | |||
| 84 | 5-(piperidin-4-yl)isothiazol-3-ol | Drug Info | [75] | |||
| 85 | 5-(piperidin-4-yl)isoxazol-3-ol | Drug Info | [76] | |||
| 86 | 5-[(1R)-1-ammonioethyl]isoxazol-3-olate | Drug Info | [55] | |||
| 87 | 5-[(1S)-1-ammonioethyl]isoxazol-3-olate | Drug Info | [55] | |||
| 88 | 6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one | Drug Info | [60] | |||
| 89 | 6-benzyl-3-ethoxycarbonyl-4-quinolone | Drug Info | [68] | |||
| 90 | 6-benzyl-3-propoxycarbonyl-4-quinolone | Drug Info | [68] | |||
| 91 | 6-benzyl-3-propylaminocarbonyl-4-quinolone | Drug Info | [68] | |||
| 92 | 6-Bromo-2-(2-nitro-phenyl)-chromen-4-one | Drug Info | [78] | |||
| 93 | 6-Bromo-2-(3-bromo-phenyl)-chromen-4-one | Drug Info | [63] | |||
| 94 | 6-Bromo-2-(3-nitro-phenyl)-chromen-4-one | Drug Info | [78] | |||
| 95 | 6-Bromo-2-(4-nitro-phenyl)-chromen-4-one | Drug Info | [78] | |||
| 96 | 6-Bromo-2-phenyl-chromen-4-one | Drug Info | [63] | |||
| 97 | 6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone | Drug Info | [68] | |||
| 98 | 6-bromo-3-ethoxycarbonyl-4-quinolone | Drug Info | [68] | |||
| 99 | 6-Chloro-2-(3-nitro-phenyl)-chromen-4-one | Drug Info | [63] | |||
| 100 | 6-Chloro-2-phenyl-chromen-4-one | Drug Info | [63] | |||
| 101 | 6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone | Drug Info | [68] | |||
| 102 | 6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone | Drug Info | [68] | |||
| 103 | 6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone | Drug Info | [68] | |||
| 104 | 6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone | Drug Info | [68] | |||
| 105 | 6-ethyl-3-i-propoxycarbonyl-4-quinolone | Drug Info | [68] | |||
| 106 | 6-ethyl-3-pentoxycarbonyl-4-quinolone | Drug Info | [68] | |||
| 107 | 6-ethyl-3-propoxycarbonyl-4-quinolone | Drug Info | [68] | |||
| 108 | 6-ethyl-3-propylaminocarbonyl-4-quinolone | Drug Info | [68] | |||
| 109 | 6-Methyl-2-oxa-spiro[4.4]nonan-1-one | Drug Info | [60] | |||
| 110 | 6-Nitro-2-(3-nitro-phenyl)-chromen-4-one | Drug Info | [79] | |||
| 111 | 7,12-Dihydro-5,7,12-triaza-indeno[1,2-a]fluorene | Drug Info | [80] | |||
| 112 | 7,12-Dihydro-7,12-diaza-indeno[1,2-a]fluorene | Drug Info | [69] | |||
| 113 | 9H-beta-Carbolin-3-ol | Drug Info | [69] | |||
| 114 | 9H-beta-Carbolin-6-ylamine | Drug Info | [56] | |||
| 115 | 9H-beta-Carboline-3-carboxylic acid ethyl ester | Drug Info | [67], [81] | |||
| 116 | 9H-beta-Carboline-3-carboxylic acid propyl ester | Drug Info | [81] | |||
| 117 | AMENTOFLAVONE | Drug Info | [82] | |||
| 118 | Barbituric acid derivative | Drug Info | [83] | |||
| 119 | Benzyl-(9H-beta-carbolin-6-yl)-amine | Drug Info | [69] | |||
| 120 | Beta-Carboline-3-carboxylic acid t-butyl ester | Drug Info | [67] | |||
| 121 | BETA-CCM | Drug Info | [84] | |||
| 122 | CGS-13767 | Drug Info | [85] | |||
| 123 | CGS-9895 | Drug Info | [86] | |||
| 124 | CI-218872 | Drug Info | [72] | |||
| 125 | Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [67] | |||
| 126 | flavone | Drug Info | [63] | |||
| 127 | GNF-PF-4421 | Drug Info | [68] | |||
| 128 | Isoquinoline-3-carboxylic acid methyl ester | Drug Info | [69] | |||
| 129 | L-655708 | Drug Info | [87] | |||
| 130 | N-(9H-beta-Carbolin-3-yl)-acetamide | Drug Info | [58] | |||
| 131 | N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide | Drug Info | [88] | |||
| 132 | N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide | Drug Info | [88] | |||
| 133 | N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide | Drug Info | [88] | |||
| 134 | N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide | Drug Info | [88] | |||
| 135 | N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide | Drug Info | [88] | |||
| 136 | N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide | Drug Info | [89] | |||
| 137 | NORHARMANE | Drug Info | [69] | |||
| 138 | NSC-73613 | Drug Info | [63] | |||
| 139 | NSC-93394 | Drug Info | [63] | |||
| 140 | Pyrrolidin-3-yl-acetic acid | Drug Info | [90] | |||
| 141 | Ridine-5-carboxylic acid ethyl ester | Drug Info | [91] | |||
| 142 | RIPAZEPAM | Drug Info | [92] | |||
| 143 | RO-054520 | Drug Info | [93] | |||
| 144 | RO-145974 | Drug Info | [94] | |||
| 145 | RO-145975 | Drug Info | [94] | |||
| 146 | RO-147437 | Drug Info | [94] | |||
| 147 | Ro-15-3505 | Drug Info | [94] | |||
| 148 | Ro-4938581 | Drug Info | [95] | |||
| 149 | RWJ-16979 | Drug Info | [96] | |||
| 150 | RY-066 | Drug Info | [97] | |||
| 151 | Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [67] | |||
| 152 | U-89267 | Drug Info | [98] | |||
| 153 | [3H]CGP27492 | Drug Info | [99] | |||
| 154 | [3H]CGS8216 | Drug Info | [85] | |||
| 155 | [3H]Ro154513 | Drug Info | [94] | |||
| Antagonist | [+] 17 Antagonist drugs | + | ||||
| 1 | Amobarbital | Drug Info | [1], [45] | |||
| 2 | Barbital | Drug Info | [1], [45] | |||
| 3 | Butabarbital | Drug Info | [1], [45], [46] | |||
| 4 | Butalbital | Drug Info | [1] | |||
| 5 | Butethal | Drug Info | [1] | |||
| 6 | Clobazam - Lundbeck | Drug Info | [1] | |||
| 7 | Ethanol | Drug Info | [1] | |||
| 8 | Ethchlorvynol | Drug Info | [1] | |||
| 9 | Hexobarbital | Drug Info | [1], [45] | |||
| 10 | Methohexital | Drug Info | [1] | |||
| 11 | Methoxyflurane | Drug Info | [1] | |||
| 12 | Methylphenobarbital | Drug Info | [1], [45] | |||
| 13 | Methyprylon | Drug Info | [1] | |||
| 14 | Nitrazepam | Drug Info | [1] | |||
| 15 | Pentobarbital | Drug Info | [1], [45] | |||
| 16 | Picrotoxin | Drug Info | [1] | |||
| 17 | Secobarbital | Drug Info | [1], [45] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | Indiplon | Drug Info | [22], [47] | |||
| Modulator | [+] 3 Modulator drugs | + | ||||
| 1 | Zaleplon | Drug Info | [49] | |||
| 2 | Zolpidem | Drug Info | [50] | |||
| 3 | EVT-201 | Drug Info | [6] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Propofol | Ligand Info | |||||
| Structure Description | Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with GABA plus propofol | PDB:6X3T | ||||
| Method | Electron microscopy | Resolution | 2.55 Å | Mutation | No | [100] |
| PDB Sequence |
DNTTVFTRIL
19 DRLLDGYDNR29 LRPGLGERVT39 EVKTDIFVTS49 FGPVSDHDME59 YTIDVFFRQS 69 WKDERLKFKG79 PMTVLRLNNL89 MASKIWTPDT99 FFHNGKKSVA109 HNMTMPNKLL 119 RITEDGTLLY129 TMRLTVRAEC139 PMHLEDFPMD149 AHACPLKFGS159 YAYTRAEVVY 169 EWTREPARSV179 VVAEDGSRLN189 QYDLLGQTVD199 SGIVQSSTGE209 YVVMTTHFHL 219 KRKIGYFVIQ229 TYLPCIMTVI239 LSQVSFWLNR249 ESVPARTVFG259 VTTVLTMTTL 269 SISARNSLPK279 VAYATAMDWF289 IAVCYAFVFS299 ALIEFATVNY309 FTKSQPARAA 319 KIDRLSRIAF329 PLLFGIFNLV339 YWATYLNR
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| Ligand Name: Zolpidem | Ligand Info | |||||
| Structure Description | Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with GABA plus Zolpidem | PDB:8DD2 | ||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [101] |
| PDB Sequence |
DNTTVFTRIL
19 DRLLDGYDNR29 LRPGLGERVT39 EVKTDIFVTS49 FGPVSDHDME59 YTIDVFFRQS 69 WKDERLKFKG79 PMTVLRLNNL89 MASKIWTPDT99 FFHNGKKSVA109 HNMTMPNKLL 119 RITEDGTLLY129 TMRLTVRAEC139 PMHLEDFPMD149 AHACPLKFGS159 YAYTRAEVVY 169 EWTREPARSV179 VVAEDGSRLN189 QYDLLGQTVD199 SGIVQSSTGE209 YVVMTTHFHL 219 KRKIGYFVIQ229 TYLPCIMTVI239 LSQVSFWLNR249 ESVPARTVFG259 VTTVLTMTTL 269 SISARNSLPK279 VAYATAMDWF289 IAVCYAFVFS299 ALIEFATVNY309 FTKSQPARAA 319 KIDRLSRIAF329 PLLFGIFNLV339 YWATYLNR
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
|
|
|
There is no similarity protein (E value < 0.005) for this target
|
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Retrograde endocannabinoid signaling | hsa04723 | Affiliated Target |
|
| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| GABAergic synapse | hsa04727 | Affiliated Target |
|
| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Taste transduction | hsa04742 | Affiliated Target |
|
| Class: Organismal Systems => Sensory system | Pathway Hierarchy | ||
| Degree | 5 | Degree centrality | 5.37E-04 | Betweenness centrality | 8.10E-04 |
|---|---|---|---|---|---|
| Closeness centrality | 1.72E-01 | Radiality | 1.27E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 2.80E+00 | Topological coefficient | 2.00E-01 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
| 1 | Neuroactive ligand-receptor interaction | |||||
| 2 | Retrograde endocannabinoid signaling | |||||
| 3 | GABAergic synapse | |||||
| 4 | Morphine addiction | |||||
| 5 | Nicotine addiction | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Ligand-gated ion channel transport | |||||
| 2 | GABA A receptor activation | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | SIDS Susceptibility Pathways | |||||
| 2 | Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell | |||||
| 3 | Iron uptake and transport | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. | |||||
| REF 2 | The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71. | |||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5338). | |||||
| REF 5 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040586. | |||||
| REF 6 | Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. | |||||
| REF 7 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 8 | Drug information of Amobarbital, 2008. eduDrugs. | |||||
| REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7137). | |||||
| REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085550. | |||||
| REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7138). | |||||
| REF 12 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076528. | |||||
| REF 13 | Drug information of Soneryl, 2008. eduDrugs. | |||||
| REF 14 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7149). | |||||
| REF 15 | Drug information of Clobazam, 2008. eduDrugs. | |||||
| REF 16 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2299). | |||||
| REF 17 | Preclinical evaluation of riluzole: assessments of ethanol self-administration and ethanol withdrawal symptoms. Alcohol Clin Exp Res. 2009 Aug;33(8):1460-8. | |||||
| REF 18 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7180). | |||||
| REF 19 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 084463. | |||||
| REF 20 | Drug information of Hexobarbital, 2008. eduDrugs. | |||||
| REF 21 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4221). | |||||
| REF 22 | Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62. | |||||
| REF 23 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7233). | |||||
| REF 24 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011559. | |||||
| REF 25 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7234). | |||||
| REF 26 | Drug information of Methoxyflurane, 2008. eduDrugs. | |||||
| REF 27 | Drug information of Methylphenobarbital, 2008. eduDrugs. | |||||
| REF 28 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7238). | |||||
| REF 29 | Nonlinear elimination of methyprylon (noludar) in an overdosed patient: correlation of clinical effects with plasma concentration. J Pharm Sci. 1991 Aug;80(8):768-71. | |||||
| REF 30 | Drug information of Nitrazepam, 2008. eduDrugs. | |||||
| REF 31 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5480). | |||||
| REF 32 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083270. | |||||
| REF 33 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4051). | |||||
| REF 34 | Drug information of Fish berry, 2008. eduDrugs. | |||||
| REF 35 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4345). | |||||
| REF 36 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 077237. | |||||
| REF 37 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4348). | |||||
| REF 38 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4346). | |||||
| REF 39 | Abecarnil enhances GABA-induced currents in acutely isolated cerebellar Purkinje cells. Neuropharmacology. 1995 Feb;34(2):157-63. | |||||
| REF 40 | ClinicalTrials.gov (NCT00380003) Efficacy Study of EVT 201 to Treat Insomnia. U.S. National Institutes of Health. | |||||
| REF 41 | Emerging drugs to treat Crohn's disease. Expert Opin Emerg Drugs. 2007 Mar;12(1):49-59. | |||||
| REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005875) | |||||
| REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001194) | |||||
| REF 44 | Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (... J Med Chem. 2005 Apr 21;48(8):3051-9. | |||||
| REF 45 | Effect of barbiturates on polyphosphoinositide biosynthesis and protein kinase C activity in synaptosomes. Neuropharmacology. 1989 Dec;28(12):1317-23. | |||||
| REF 46 | Hypnotic drugs. Med Lett Drugs Ther. 2000 Aug 7;42(1084):71-2. | |||||
| REF 47 | Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17. | |||||
| REF 48 | 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7. | |||||
| REF 49 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 50 | Zolpidem, a selective GABA(A) receptor alpha1 subunit agonist, induces comparable Fos expression in oxytocinergic neurons of the hypothalamic paraventricular and accessory but not supraoptic nuclei in the rat.Brain Res Bull.2006 Dec 11;71(1-3):200-7. | |||||
| REF 51 | Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carbolin... J Med Chem. 1990 Mar;33(3):1062-9. | |||||
| REF 52 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. J Med Chem. 1999 Apr 8;42(7):1123-44. | |||||
| REF 53 | (Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics. J Med Chem. 1988 Jun;31(6):1220-6. | |||||
| REF 54 | ( )-2-amino-2-thiazoline-4-ethanoic acid; a novel, specific GABAA receptor agonist. Bioorg. Med. Chem. Lett. 1(5):247-248 (1991). | |||||
| REF 55 | gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. J Med Chem. 1981 Dec;24(12):1377-83. | |||||
| REF 56 | Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists. J Med Chem. 1987 Apr;30(4):750-3. | |||||
| REF 57 | Benzodiazepine receptor binding activity of 6,9-disubstituted purines. J Med Chem. 1989 May;32(5):1020-4. | |||||
| REF 58 | 3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam. J Med Chem. 1985 Jun;28(6):824-8. | |||||
| REF 59 | Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives. J Med Chem. 1992 Jun 12;35(12):2214-20. | |||||
| REF 60 | Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant ... J Med Chem. 1994 Jan 21;37(2):275-86. | |||||
| REF 61 | Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ... J Med Chem. 1988 Jan;31(1):1-3. | |||||
| REF 62 | Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. J Med Chem. 2006 Mar 23;49(6):1855-66. | |||||
| REF 63 | Synthesis of halogenated/nitrated flavone derivatives and evaluation of their affinity for the central benzodiazepine receptor, Bioorg. Med. Chem. Lett. 7(15):2003-2008 (1997). | |||||
| REF 64 | Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand. J Med Chem. 1996 Jul 19;39(15):2915-21. | |||||
| REF 65 | Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. J Med Chem. 1996 Jul 5;39(14):2844-51. | |||||
| REF 66 | Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach. J Med Chem. 1992 Oct 30;35(22):4001-10. | |||||
| REF 67 | Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents f... Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. | |||||
| REF 68 | 4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore mod... J Med Chem. 2006 Apr 20;49(8):2526-33. | |||||
| REF 69 | Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore. J Med Chem. 1988 Sep;31(9):1854-61. | |||||
| REF 70 | Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site. J Med Chem. 1990 Sep;33(9):2343-57. | |||||
| REF 71 | N-2 methylated quaternary derivatives of beta-carboline-3-carboxylates inhibit acetylcholinesterase in vitroO, Bioorg. Med. Chem. Lett. 3(12):2831-2836 (1993). | |||||
| REF 72 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. J Med Chem. 1994 Dec 23;37(26):4576-80. | |||||
| REF 73 | Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of ga... J Med Chem. 2006 Jul 13;49(14):4442-6. | |||||
| REF 74 | Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relatio... J Med Chem. 2010 Apr 22;53(8):3417-21. | |||||
| REF 75 | Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology. J Med Chem. 2006 Feb 23;49(4):1388-96. | |||||
| REF 76 | Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. J Med Chem. 2005 Jan 27;48(2):427-39. | |||||
| REF 77 | Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) a... J Med Chem. 1998 Jul 2;41(14):2537-52. | |||||
| REF 78 | 6-Bromo-3 nitroflavone, a new high affinity benzodiazepine receptor agonist recognizes two populations of cerebral cortical binding sites, Bioorg. Med. Chem. Lett. 7(3):373-378 (1997). | |||||
| REF 79 | 6,3'-Dinitroflavone, a novel high affinity ligand for the benzodiazepine receptor with potent anxiolytic properties, Bioorg. Med. Chem. Lett. 5(22):2717-2720 (1995). | |||||
| REF 80 | Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands. J Med Chem. 1987 Mar;30(3):456-8. | |||||
| REF 81 | beta-Carbolines as benzodiazepine receptor ligands. 1. Synthesis and benzodiazepine receptor interaction of esters of beta-carboline-3-carboxylic a... J Med Chem. 1983 Apr;26(4):499-503. | |||||
| REF 82 | Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4. | |||||
| REF 83 | Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. | |||||
| REF 84 | Synthetic routes to 4-amino-3-carboxy-beta-carboline derivatives: incidental formation of novel furo[3,4-c]-beta-carbolin-2-ones displaying high af... J Med Chem. 1995 Jan 6;38(1):189-98. | |||||
| REF 85 | Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones. J Med Chem. 1991 Jan;34(1):281-90. | |||||
| REF 86 | 1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding. J Med Chem. 1987 Oct;30(10):1737-42. | |||||
| REF 87 | 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor li... J Med Chem. 2004 Mar 25;47(7):1807-22. | |||||
| REF 88 | Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-... J Med Chem. 2007 Apr 5;50(7):1627-34. | |||||
| REF 89 | Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular mo... J Med Chem. 2001 Jul 5;44(14):2286-97. | |||||
| REF 90 | Orally active and potent inhibitors of gamma-aminobutyric acid uptake. J Med Chem. 1985 May;28(5):653-60. | |||||
| REF 91 | Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. J Med Chem. 1989 Dec;32(12):2561-73. | |||||
| REF 92 | Synthesis and interaction of 5-(substituted-phenyl)-3-methyl-6,7-dihydropyrazolo[4,3-e] [1,4]diazepin-8(7H)-ones with benzodiazepine receptors in r... J Med Chem. 1985 May;28(5):683-5. | |||||
| REF 93 | Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. J Med Chem. 1988 Dec;31(12):2235-46. | |||||
| REF 94 | Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepin... J Med Chem. 1993 Apr 16;36(8):1001-6. | |||||
| REF 95 | The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment... Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. | |||||
| REF 96 | Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors. J Med Chem. 1995 Jan 6;38(1):16-20. | |||||
| REF 97 | Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines a... J Med Chem. 1998 Oct 8;41(21):4130-42. | |||||
| REF 98 | Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. J Med Chem. 1994 Mar 18;37(6):758-68. | |||||
| REF 99 | Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312. | |||||
| REF 100 | Shared structural mechanisms of general anaesthetics and benzodiazepines. Nature. 2020 Sep;585(7824):303-308. | |||||
| REF 101 | Structural and dynamic mechanisms of GABA(A) receptor modulators with opposing activities. Nat Commun. 2022 Aug 6;13(1):4582. | |||||
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